Gusacitinib
Based on 1 publication(s) in Google Scholar
Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma.
For research use only. We do not sell to patients.
- Purity: 99.63%
- CAS No.: 1425381-60-7
- Formula: C24H28N8O2
- Molecular Weight:460.53
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Gusacitinib
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Biological Activity
IC50: 5-46 nM (SYK, JAK)[2].
Gusacitinib shows anti-proliferative activity in a broad panel of human cancer cell lines including DHL6, DHL4, OCI-LY10, H929, Pfeiffer, HT-1376, and Lovo, suggesting activity in both solid and hematological tumor types[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Gusacitinib shows a favorable safety profile in rat and dog toxicology studies[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1425381-60-7
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Appearance Solid
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Molecular Weight 460.53
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Formula C24H28N8O2
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Color Light yellow to yellow
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SMILES
N#CCC1CCN(C2=NC(NC3=CC=C(N4CCC(O)CC4)C=C3)=C5C(C=NNC5=O)=N2)CC1
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Synonyms
ASN-002
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 100 mg/mL (217.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (3.63 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (3.63 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (762 KB)
- English - EN (762 KB)
- Français - FR (762 KB)
- Deutsch - DE (762 KB)
- Norwegian - NO (762 KB)
- Español - ES (762 KB)
- Swedish - SV (762 KB)
- Italian - IT (762 KB)
- Korean - KR (762 KB)
- Portuguese - PT (762 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1714 mL | 10.8571 mL | 21.7141 mL | 54.2853 mL |
| 5 mM | 0.4343 mL | 2.1714 mL | 4.3428 mL | 10.8571 mL | |
| 10 mM | 0.2171 mL | 1.0857 mL | 2.1714 mL | 5.4285 mL | |
| 15 mM | 0.1448 mL | 0.7238 mL | 1.4476 mL | 3.6190 mL | |
| 20 mM | 0.1086 mL | 0.5429 mL | 1.0857 mL | 2.7143 mL | |
| 25 mM | 0.0869 mL | 0.4343 mL | 0.8686 mL | 2.1714 mL | |
| 30 mM | 0.0724 mL | 0.3619 mL | 0.7238 mL | 1.8095 mL | |
| 40 mM | 0.0543 mL | 0.2714 mL | 0.5429 mL | 1.3571 mL | |
| 50 mM | 0.0434 mL | 0.2171 mL | 0.4343 mL | 1.0857 mL | |
| 60 mM | 0.0362 mL | 0.1810 mL | 0.3619 mL | 0.9048 mL | |
| 80 mM | 0.0271 mL | 0.1357 mL | 0.2714 mL | 0.6786 mL | |
| 100 mM | 0.0217 mL | 0.1086 mL | 0.2171 mL | 0.5429 mL |
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